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Direct C‐3‐Arylations of 1 H ‐Indazoles
Author(s) -
BenYahia Ali,
Naas Mohammed,
El Kazzouli Saïd,
Essassi El Mokhtar,
Guillaumet Gérald
Publication year - 2012
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201200860
Subject(s) - chemistry , intermolecular force , ligand (biochemistry) , catalysis , aryl , phenanthroline , solvent , medicinal chemistry , combinatorial chemistry , base (topology) , stereochemistry , organic chemistry , molecule , receptor , mathematical analysis , biochemistry , alkyl , mathematics
The first example of intermolecular C–H arylation of substituted 1 H ‐indazoles is reported. Various 1‐substituted indazoles were used as starting materials, and (hetero)aryl bromides and iodides were investigated as coupling partners. Different reaction conditions were investigated. The best results were obtained using Pd(OAc) 2 as catalyst, 1,10‐phenanthroline as ligand, K 2 CO 3 as base, and DMA as solvent. The crucial role of the ligand on the C–H arylation of substituted 1 H ‐indazoles is highlighted.